Cirsilineol inhibits proliferation of cancer cells by inducing apoptosis via mitochondrial pathway.
Cirsilineol (4',5-dihydroxy-3',6,7-trimethoxyflavone) is a compound isolated from the herb of Artemisia vestita Wall (Compositae). In this study, we aimed at examining the anti-proliferative activity of cirsilineol against multiple types of cancer cells and the underlying mechanisms. Cirsilineol significantly inhibited proliferation of Caov-3, Skov-3, PC3 and Hela cells in a concentration-dependent manner. The compound also dose-dependently induced apoptosis in Caov-3 cells, as determined by annexin V/propidium iodide staining. Besides, cirsilineol induced a remarkable change in mitochondrial membrane potential and caused release of cytochrome c to cytosol. Furthermore, the compound caused a marked activation of capase-3, caspase-9 and poly (ADP-ribose) polymerase (PARP). These results suggested that the induction of apoptosis via the mitochondrial pathway was involved in the anti-proliferative activity of cirsilineol against cancer cells.
Sheng
Xia
X
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, 22 Han Kou Road, Nanjing 210093, China.
Sun
Yang
Y
Yin
Ye
Y
Chen
Ting
T
Xu
Qiang
Q
D017209:Apoptosis / Q000187:drug effects*; D019306:Artemisia / Q000737:chemistry*; D053148:Caspase 3 / Q000187:drug effects / Q000378:metabolism; D053453:Caspase 9 / Q000187:drug effects / Q000378:metabolism; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D045304:Cytochromes c / Q000187:drug effects / Q000378:metabolism; D047309:Flavones / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D053078:Membrane Potential, Mitochondrial / Q000187:drug effects; D011065:Poly(ADP-ribose) Polymerases / Q000187:drug effects / Q000378:metabolism
D047309:Flavones; C057618:cirsilineol; D045304:Cytochromes c; D011065:Poly(ADP-ribose) Polymerases; D053148:Caspase 3; D053453:Caspase 9